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Pregled bibliografske jedinice broj: 1218865

Synthesis and biological activity of newly designed 2-benzothienyl and 2-bithieny amidino- substituted benzazole derivatives


Racané, Livio; Cindrić, Maja; Mehić, Emina; Karminski-Zamola, Grace; Zlatić, Katarina; Kralj, Marijeta; Taylor, Martin C.; Kelly, John M., Hranjec, Marijana;
Synthesis and biological activity of newly designed 2-benzothienyl and 2-bithieny amidino- substituted benzazole derivatives // 8th EuChemS Chemistry Congress: Book of abstracts / Silva, Artur M. S. ; Galvão, Adelino M. ; Machado, Bruno F. ; Faria, Joaquim L. (ur.).
Lisabon: Sociedade Portuguesa de Química, 2022. str. 609-609 (poster, međunarodna recenzija, sažetak, znanstveni)


CROSBI ID: 1218865 Za ispravke kontaktirajte CROSBI podršku putem web obrasca

Naslov
Synthesis and biological activity of newly designed 2-benzothienyl and 2-bithieny amidino- substituted benzazole derivatives

Autori
Racané, Livio ; Cindrić, Maja ; Mehić, Emina ; Karminski-Zamola, Grace ; Zlatić, Katarina ; Kralj, Marijeta ; Taylor, Martin C. ; Kelly, John M., Hranjec, Marijana ;

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
8th EuChemS Chemistry Congress: Book of abstracts / Silva, Artur M. S. ; Galvão, Adelino M. ; Machado, Bruno F. ; Faria, Joaquim L. - Lisabon : Sociedade Portuguesa de Química, 2022, 609-609

ISBN
978-989-8124-35-7

Skup
8th EuChemS Chemistry Congress (ECC8)

Mjesto i datum
Lisabon, Portugal, 28.08.2022. - 01.09.2022

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
benzothiazole ; benzimidazole ; amidine ; synthesis ; biological activity

Sažetak
It is well known that cationic amidines, placed usually at the termini of the molecule, are structural parts of numerous compounds of biological interest. Their main function is the interaction with potential biological targets and formation of the stable complex with biological molecules. On the other hand, benzimidazoles and benzothiazoles as one of the most important heterocyclic nitrogen scaffolds have great biological importance and thus become unavoidable structural motifs in the rational design of novel drugs. In our recent studies we have proved that by engrafting amidine extremities as positively charged substituents at the end of the heteroaromatic substructures we could significantly improve the antiproliferative [1, 2] as well as antitrypanosomal activities [3]. Herein we present the synthesis of newly designed 2-benzothienyl and 2-bithienyl benzimidazole/benzothiazole derivatives bearing either acyclic unsubstituted and isopropyl amidine moiety, as well as cyclic 2-imidazolinyl and 3, 4, 5, 6-tetrahydropyrimidin-2-yl amidine moiety. All prepared compounds were tested for their antiproliferative activity on six human cancer cell lines (HCT116, H460, MCF-7, PC3, HeLa, SW620) and non-tumour cell line HEK 293, while antitrypanosomal activity was tested on protozoan parasite Trypanosoma brucei. Some of tested compounds showed strong and selective antiproliferative activity against H 460 cells in submicromolar range of inhibitory concentrations. Obtained results revealed that benzothiazole derivatives were more active in comparison to their benzimidazole analogues. Additionally, we can conclude that also the type of the amidine group has strong influence on the biological activity.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Biologija



POVEZANOST RADA


Projekti:
HRZZ-IP-2018-01-4379 - Istraživanje antioksidativnog djelovanja benzazolskog skeleta u dizajnu novih antitumorskih agensa (AntioxPot) (Hranjec, Marijana, HRZZ - 2018-01) ( CroRIS)

Ustanove:
Institut "Ruđer Bošković", Zagreb,
Tekstilno-tehnološki fakultet, Zagreb,
Fakultet kemijskog inženjerstva i tehnologije, Zagreb

Poveznice na cjeloviti tekst rada:

Pristup cjelovitom tekstu rada www.spq.pt

Citiraj ovu publikaciju:

Racané, Livio; Cindrić, Maja; Mehić, Emina; Karminski-Zamola, Grace; Zlatić, Katarina; Kralj, Marijeta; Taylor, Martin C.; Kelly, John M., Hranjec, Marijana;
Synthesis and biological activity of newly designed 2-benzothienyl and 2-bithieny amidino- substituted benzazole derivatives // 8th EuChemS Chemistry Congress: Book of abstracts / Silva, Artur M. S. ; Galvão, Adelino M. ; Machado, Bruno F. ; Faria, Joaquim L. (ur.).
Lisabon: Sociedade Portuguesa de Química, 2022. str. 609-609 (poster, međunarodna recenzija, sažetak, znanstveni)
Racané, L., Cindrić, M., Mehić, E., Karminski-Zamola, G., Zlatić, K., Kralj, M., Taylor, M., Kelly, John M., Hranjec, Marijana & (2022) Synthesis and biological activity of newly designed 2-benzothienyl and 2-bithieny amidino- substituted benzazole derivatives. U: Silva, A., Galvão, A., Machado, B. & Faria, J. (ur.)8th EuChemS Chemistry Congress: Book of abstracts.
@article{article, author = {Racan\'{e}, Livio and Cindri\'{c}, Maja and Mehi\'{c}, Emina and Karminski-Zamola, Grace and Zlati\'{c}, Katarina and Kralj, Marijeta and Taylor, Martin C.}, year = {2022}, pages = {609-609}, keywords = {benzothiazole, benzimidazole, amidine, synthesis, biological activity}, isbn = {978-989-8124-35-7}, title = {Synthesis and biological activity of newly designed 2-benzothienyl and 2-bithieny amidino- substituted benzazole derivatives}, keyword = {benzothiazole, benzimidazole, amidine, synthesis, biological activity}, publisher = {Sociedade Portuguesa de Qu\'{\i}mica}, publisherplace = {Lisabon, Portugal} }
@article{article, author = {Racan\'{e}, Livio and Cindri\'{c}, Maja and Mehi\'{c}, Emina and Karminski-Zamola, Grace and Zlati\'{c}, Katarina and Kralj, Marijeta and Taylor, Martin C.}, year = {2022}, pages = {609-609}, keywords = {benzothiazole, benzimidazole, amidine, synthesis, biological activity}, isbn = {978-989-8124-35-7}, title = {Synthesis and biological activity of newly designed 2-benzothienyl and 2-bithieny amidino- substituted benzazole derivatives}, keyword = {benzothiazole, benzimidazole, amidine, synthesis, biological activity}, publisher = {Sociedade Portuguesa de Qu\'{\i}mica}, publisherplace = {Lisabon, Portugal} }




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